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Bioorg Med Chem. 2016 Nov 1;24(21):5148-5157. doi: 10.1016/j.bmc.2016.08.032. Epub 2016 Aug 23.

Blood-brain barrier permeability of ginkgolide: Comparison of the behavior of PET probes 7α-[18F]fluoro- and 10-O-p-[11C]methylbenzyl ginkgolide B in monkey and rat brains.

Author information

1
Division of Bio-Function Dynamics Imaging, RIKEN Center for Life Science Technologies (CLST), 6-7-3 Minatojima-minamimachi, Chuo-ku, Kobe 650-0047, Japan. Electronic address: hisashi.doi@riken.jp.
2
PET Medical Application Group, Central Research Laboratory, Hamamatsu Photonics K.K., 5000 Hirakuchi, Hamakita-ku, Hamamatsu 434-8601, Japan. Electronic address: satoken@crl.hpk.co.jp.
3
Department of Lipid Signaling, Research Institute, National Center for Global Health and Medicine, 1-21-1 Toyama, Shinjuku-ku, Tokyo 162-8655, Japan. Electronic address: hshindou-tky@umin.net.
4
Division of Regeneration and Advanced Medical Science, Graduate School of Medicine, Gifu University, 1-1 Yanagido, Gifu 501-1194, Japan. Electronic address: kesumi@dwti.co.jp.
5
Division of Regeneration and Advanced Medical Science, Graduate School of Medicine, Gifu University, 1-1 Yanagido, Gifu 501-1194, Japan. Electronic address: hirokok@gifu-u.ac.jp.
6
Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, 2-3-10 Kanda-Surugadai, Chiyoda-ku, Tokyo 101-0062, Japan. Electronic address: thosoya.cb@tmd.ac.jp.
7
Division of Bio-Function Dynamics Imaging, RIKEN Center for Life Science Technologies (CLST), 6-7-3 Minatojima-minamimachi, Chuo-ku, Kobe 650-0047, Japan. Electronic address: yywata@riken.jp.
8
Department of Immunology, Akita University Graduate School of Medicine, 1-1-1 Hondo, Akita 010-8543, Japan. Electronic address: satishii@med.akita-u.ac.jp.
9
PET Center, Central Research Laboratory, Hamamatsu Photonics K.K., 5000 Hirakuchi, Hamakita-ku, Hamamatsu 434-8601, Japan. Electronic address: tsukada@crl.hpk.co.jp.
10
Department of Chemistry, Columbia University, 3000 Broadway, New York, NY 10027, USA. Electronic address: kn5@columbia.edu.
11
Department of Clinical and Experimental Neuroimaging, National Center for Geriatrics and Gerontology, Obu, Aichi 474-8511, Japan. Electronic address: suzukims@ncgg.go.jp.

Abstract

The blood-brain barrier permeability of ginkgolide B was examined using positron emission tomography (PET) probes of a 18F-incorporated ginkgolide B ([18F]-2) and a 11C-incorporated methylbenzyl-substituted ginkgolide B ([11C]-3). PET studies in monkeys showed low uptake of [18F]-2 into the brain, but small amounts of [11C]-3 were accumulated in the parenchyma. Furthermore, when cyclosporine A was preadministered to rats, the accumulation of [18F]-2 in the rat brain did not significantly change, however, the accumulation of [11C]-3 was five times higher than that in the control rat. These results provide effective approaches for investigating the drug potential of ginkgolides.

KEYWORDS:

Blood–brain barrier; C-[(11)C]methylation; Ginkgolide B; PET; Platelet-activating factor

PMID:
27614918
DOI:
10.1016/j.bmc.2016.08.032
[Indexed for MEDLINE]

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